Dacomitinib (PF299804, PF299) , ≥99% , 1110813-31-4

Synonym(s):
(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide;PF-00299804;PF-00299804-03;PF-299

CAS NO.：1110813-31-4

Empirical Formula: C24H25ClFN5O2

Molecular Weight: 469.94

MDL number: MFCD19443734

Pack Size	Price	Stock	Quantity
5MG	RMB95.20	In Stock
10MG	RMB143.20	In Stock
50MG	RMB559.20	In Stock
250MG	RMB1599.20	In Stock
others			Enquire

Update time: 2022-07-08

PRODUCT Properties

Melting point:	184-187°C
Boiling point:	665.7±55.0 °C(Predicted)
Density	1.344
storage temp.	Refrigerator
solubility	DMSO (Slightly), Methanol (Slightly, Heated)
form	White solid.
pka	12.05±0.43(Predicted)
color	White to Pale Yellow
InChIKey	LVXJQMNHJWSHET-AATRIKPKSA-N
SMILES	C(NC1C(OC)=CC2C(C=1)=C(NC1=CC=C(F)C(Cl)=C1)N=CN=2)(=O)/C=C/CN1CCCCC1

Description and Uses

The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer. PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC₅₀s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors. At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.

Dacomitinib is an Erb-inhibitor, or an inhibitor of the members of the epidermal growth factor receptor family. Used as an ant-cancer agent due to observation of over-expressed epidermal growth factor receptor in nearly all cases of squamous cell carcinoma in the head and neck.